Design and synthesis of novel dual-cyclic RGD peptides for αvβ3 integrin targeting

[Display omitted] The specific binding of RGD cyclic peptide with integrin αvβ3 attracts great research interest for tumor-targeting drug delivery. Herein, we designed and synthesized a series of dual-ring RGD-peptide derivatives as a drug carrier for αvβ3 targeting. Three novel peptides showed exce...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2019-04, Vol.29 (7), p.896-900
Main Authors: Liu, Junjie, Cheng, Xiaozhong, Tian, Xiaobo, Guan, Dongliang, Ao, Jiwei, Wu, Zhimeng, Huang, Wei, Le, Zhiping
Format: Article
Language:English
Subjects:
Adhesion inhibition
Cyclo(RGDfK)
RGD cyclic peptide
Tumor-targeting
αvβ3 integrin
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Summary:[Display omitted] The specific binding of RGD cyclic peptide with integrin αvβ3 attracts great research interest for tumor-targeting drug delivery. Herein, we designed and synthesized a series of dual-ring RGD-peptide derivatives as a drug carrier for αvβ3 targeting. Three novel peptides showed excellent cell adhesion inhibition effect, in which, P3 exhibited 7-fold enhancement in IC50 compared with cyclo(RGDfK). Drug-loaded cytotoxicity experiment and imaging experiment indicated that such dual-cyclic RGD peptides have good tumor targeting effects. This work provides a new strategy for the design of novel RGD peptides.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2019.01.043